蛋白激酶活性及抑制性检测研究进展

Recent progress in monitoring the activity and inhibitor of protein kinase activity

蛋白激酶催化蛋白磷酸化是一种非常重要的蛋白质翻译后修饰方式,能够调节细胞内大多数蛋白的功能,在众多生理过程中发挥着至关重要的作用。磷酸化过程的异常以及激酶的过度表达往往与许多疾病密切相关,如癌症、糖尿病和老年痴呆症。因而,测定蛋白激酶的活性及筛选蛋白激酶抑制剂对基础生物医学研究和酶靶药物的开发是非常重要的。近年来,研究工作者们采用电化学法、比色法以及荧光检测法等方法研究了对蛋白激酶活性及抑制性的检测。该文回顾了蛋白激酶活性测定及抑制性检测的研究进展,主要关注了荧光检测法的应用,并对其未来的发展进行展望。

Protein phosphorylation catalyzed by protein kinase is one of the most important post-translational modifications, which adjusts the function of most proteins in cells and plays a significant regulatory role in many vital biological processes. Aberrant protein-phosphorylation states and kinase activity are closely associated with many human diseases, including cancer, diabetes and Alzheimer＇s disease. Thus, detecting the kinase activity and inhibitor screening are essential for fundamental biochemical research and kinase-targeted drug discovery. Recently, utilizing electrochemical, colorimetrlc and fluorescence techniques, researchers have developed different methods for monitoring the activity and inhibition of protein kinase. This article reviews the recent advances in the development of assays for protein kinase activity and inhibition, mainly focused assays based on fluorescence methods, and then offers perspectives on future developments.